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- 详细信息
- 文献和实验
- 技术资料
- 保存条件:
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名:
AZD0364
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
2097416-76-5
- 规格:
10 mM * 1 mL/1 mg/5 mg/10 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥3046.0 |
|---|---|---|---|
| 规格: | 1 mg | 产品价格: | ¥1173.0 |
| 规格: | 5 mg | 产品价格: | ¥2800.0 |
| 规格: | 10 mg | 产品价格: | ¥4480.0 |
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Tizaterkib
CAS No. : 2097416-76-5
MCE 国际站:Tizaterkib
产品活性:Tizaterkib (AZD0364) 是一种有效的选择性 ERK2 抑制剂,IC50 为 0.6 nM。详细信息请参考专利文献 WO2017080979A1 中的化合物 example 18。
研究领域:MAPK/ERK Pathway | Stem Cell/Wnt
作用靶点:ERK
In Vitro: Tizaterkib is measured in the ERK2 mass spectrometry and A375 phospho-p90RSK assays with IC50s of 0.6 nM and 5.7 nM, respectively. Tizaterkib can inhibit the growth of a panel of cancer cell lines (A549, H2122, H2009, and Calu6 cell lines) with KRAS mutations as a monotherapy and this effect is synergistically enhanced by treatment with Selumetinib.
In Vivo: Tumor growth inhibition by Tizaterkib ethanesulfonic acid (Example 18a) in combination with MEK inhibitor Selumetinib is measured. Studies are performed in the A549 xenograft model. Selumetinib is dosed twice daily (BiD) 8 hours apart and Tizaterkib ethanesulfonic acid is dosed once daily (QD) 4 hours after the first Selumetinib dose. Both compounds are dosed continuously for 3 weeks. Both vehicles are dosed in the vehicle group. Both Selumetinib and Tizaterkib ethanesulfonic acid reduce tumor growth relative to vehicle only control. The combination of Selumetinib and Tizaterkib ethanesulfonic acid results in a reduction in tumor growth.
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文献和实验动物种类 肠 道 长 度 单位 全长 小肠 盲肠 大肠 狗 m 2.2-5
中性粒细胞( GRAN ) 绝对值:( 18-64 ) ×109/L 百分率 : 46.0-76.5% 中性粒细胞( GRAN ) 绝对值:( 18-64 ) ×109/L 百分率 : 46.0-76
Fluorescence In Situ Hybridization
mixture at 76ºC, 5 min Incubate at 37ºC for 30-60min, competition Optional: Co-denaturation Apply probes to slide and denature at 80ºC on a heat block for 2-5 minutes HYBRIDIZATION Apply probes to dried slide Seal with rubber cement
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